JPH0328404B2 - - Google Patents
Info
- Publication number
- JPH0328404B2 JPH0328404B2 JP56177323A JP17732381A JPH0328404B2 JP H0328404 B2 JPH0328404 B2 JP H0328404B2 JP 56177323 A JP56177323 A JP 56177323A JP 17732381 A JP17732381 A JP 17732381A JP H0328404 B2 JPH0328404 B2 JP H0328404B2
- Authority
- JP
- Japan
- Prior art keywords
- nifedipine
- formulation
- solid solution
- preparation
- present
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 claims description 80
- 239000006104 solid solution Substances 0.000 claims description 61
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 claims description 58
- 229960001597 nifedipine Drugs 0.000 claims description 58
- 238000002360 preparation method Methods 0.000 claims description 46
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 32
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 32
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 29
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 29
- 239000010419 fine particle Substances 0.000 claims description 19
- 238000000576 coating method Methods 0.000 claims description 12
- 239000000243 solution Substances 0.000 claims description 12
- 239000011248 coating agent Substances 0.000 claims description 10
- 238000004519 manufacturing process Methods 0.000 claims description 8
- 239000004503 fine granule Substances 0.000 claims description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 5
- 239000008101 lactose Substances 0.000 claims description 5
- 229920000609 methyl cellulose Polymers 0.000 claims description 5
- 239000001923 methylcellulose Substances 0.000 claims description 5
- 235000010981 methylcellulose Nutrition 0.000 claims description 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 4
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 4
- 239000002245 particle Substances 0.000 claims description 4
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims description 2
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- 239000003232 water-soluble binding agent Substances 0.000 claims description 2
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 3
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 3
- 235000001727 glucose Nutrition 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 77
- 230000000052 comparative effect Effects 0.000 description 29
- 238000004090 dissolution Methods 0.000 description 16
- 239000000843 powder Substances 0.000 description 11
- 238000000034 method Methods 0.000 description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
- 238000005469 granulation Methods 0.000 description 7
- 230000003179 granulation Effects 0.000 description 7
- 238000003860 storage Methods 0.000 description 7
- 238000012360 testing method Methods 0.000 description 7
- 239000008280 blood Substances 0.000 description 5
- 210000004369 blood Anatomy 0.000 description 5
- 238000007922 dissolution test Methods 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 239000003960 organic solvent Substances 0.000 description 5
- 206010002383 Angina Pectoris Diseases 0.000 description 4
- FHHZOYXKOICLGH-UHFFFAOYSA-N dichloromethane;ethanol Chemical compound CCO.ClCCl FHHZOYXKOICLGH-UHFFFAOYSA-N 0.000 description 4
- 239000007921 spray Substances 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 3
- 241000282472 Canis lupus familiaris Species 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000010828 elution Methods 0.000 description 2
- 235000021189 garnishes Nutrition 0.000 description 2
- 229940031702 hydroxypropyl methylcellulose 2208 Drugs 0.000 description 2
- 238000005096 rolling process Methods 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- XINQFOMFQFGGCQ-UHFFFAOYSA-L (2-dodecoxy-2-oxoethyl)-[6-[(2-dodecoxy-2-oxoethyl)-dimethylazaniumyl]hexyl]-dimethylazanium;dichloride Chemical compound [Cl-].[Cl-].CCCCCCCCCCCCOC(=O)C[N+](C)(C)CCCCCC[N+](C)(C)CC(=O)OCCCCCCCCCCCC XINQFOMFQFGGCQ-UHFFFAOYSA-L 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 206010025476 Malabsorption Diseases 0.000 description 1
- 208000004155 Malabsorption Syndromes Diseases 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 241000978776 Senegalia senegal Species 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical class [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- ULUAUXLGCMPNKK-UHFFFAOYSA-N Sulfobutanedioic acid Chemical compound OC(=O)CC(C(O)=O)S(O)(=O)=O ULUAUXLGCMPNKK-UHFFFAOYSA-N 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 150000008051 alkyl sulfates Chemical class 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000008199 coating composition Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000005034 decoration Methods 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000009506 drug dissolution testing Methods 0.000 description 1
- 238000007908 dry granulation Methods 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 238000004817 gas chromatography Methods 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000000304 vasodilatating effect Effects 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP17732381A JPS5877811A (ja) | 1981-11-04 | 1981-11-04 | 安定な易吸収性ニフエジピン製剤の製法 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP17732381A JPS5877811A (ja) | 1981-11-04 | 1981-11-04 | 安定な易吸収性ニフエジピン製剤の製法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5877811A JPS5877811A (ja) | 1983-05-11 |
| JPH0328404B2 true JPH0328404B2 (hu) | 1991-04-19 |
Family
ID=16028964
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP17732381A Granted JPS5877811A (ja) | 1981-11-04 | 1981-11-04 | 安定な易吸収性ニフエジピン製剤の製法 |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5877811A (hu) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7432392B2 (en) | 2003-08-29 | 2008-10-07 | Japan Tobacco Inc. | Ester derivatives and medical use thereof |
| WO2010137888A2 (ko) | 2009-05-27 | 2010-12-02 | 주식회사 삼양사 | 생체이용률이 향상된 난용성 약물 함유 미립구 및 그 제조 방법 |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3318649A1 (de) * | 1983-05-21 | 1984-11-22 | Bayer Ag, 5090 Leverkusen | Zweiphasenformulierung |
| JPS6038322A (ja) * | 1983-08-11 | 1985-02-27 | Fujisawa Pharmaceut Co Ltd | ジヒドロピリジンａ物質含有易溶性固形製剤 |
| SE457326B (sv) * | 1986-02-14 | 1988-12-19 | Lejus Medical Ab | Foerfarande foer framstaellning av en snabbt soenderfallande kaerna innehaallande bl a mikrokristallin cellulosa |
| CA2328085C (en) | 1998-04-10 | 2006-08-22 | Mitsubishi Chemical Corporation | Solid dispersion containing sialic acid derivative |
| JP2002138034A (ja) * | 2000-10-27 | 2002-05-14 | Kyoto Pharmaceutical Industries Ltd | 苦味マスキングチュアブル錠およびその製造方法 |
| JP4644397B2 (ja) | 2001-09-05 | 2011-03-02 | 信越化学工業株式会社 | 難溶性薬物を含む医薬用固形製剤の製造方法 |
| JP6838446B2 (ja) * | 2017-03-22 | 2021-03-03 | ニプロ株式会社 | トルバプタン製剤およびその製造方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS542316A (en) * | 1977-06-07 | 1979-01-09 | Yamanouchi Pharmaceut Co Ltd | Solid pharmaceutical composition containing nifedipene |
-
1981
- 1981-11-04 JP JP17732381A patent/JPS5877811A/ja active Granted
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS542316A (en) * | 1977-06-07 | 1979-01-09 | Yamanouchi Pharmaceut Co Ltd | Solid pharmaceutical composition containing nifedipene |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7432392B2 (en) | 2003-08-29 | 2008-10-07 | Japan Tobacco Inc. | Ester derivatives and medical use thereof |
| WO2010137888A2 (ko) | 2009-05-27 | 2010-12-02 | 주식회사 삼양사 | 생체이용률이 향상된 난용성 약물 함유 미립구 및 그 제조 방법 |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5877811A (ja) | 1983-05-11 |
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